Home Protein Tyrosine Kinase EGFR inhibitor RG 13022

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RG 13022 EGFR inhibitor

Cat.No.S2115

RG 13022 (Tyrphostin RG13022) inhibits the autophosphorylation reaction of the EGF receptor in immunoprecipitates with IC50 of 4 µM.
RG 13022 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 266.29

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Quality Control

Batch: S211501 DMSO]53 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.28%
99.28

Chemical Information, Storage & Stability

Molecular Weight 266.29 Formula

C16H14N2O2

 

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 136831-48-6 -- Storage of Stock Solutions

Synonyms Tyrphostin RG13022 Smiles COC1=C(C=C(C=C1)C=C(C#N)C2=CN=CC=C2)OC

Solubility

In vitro
Batch:

DMSO : 53 mg/mL (199.03 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
EGFR [1]
(Cell-free assay)
4 μM
In vitro

RG-13022 inhibits autophosphorylation of the EGF-receptor in HER 14 cells after an overnight incubation.The IC50 of RG-13022 is 5 μM. RG-13022 inhibits colony formation and DNA synthesis by HER 14 cells, which are stimulated by 50 ng/mL EGF, in a dose-dependent manner. The IC50 for RG-13022 is 1 μM for HER 14 colony formation and 3 μM for HER 14 DNA synthesis. RG-13022 also suppresses colony formation and DNA synthesis by EGF-stimulated MH-85 cells in a dose-dependent manner. The IC50 for RG-13022 on MH-85 cells is 7 μM for colony formation and 1.5 μM for DNA synthesis.[1].
In vivo

RG-13022 (400 μg/mouse/day) significantly inhibits MH-85 tumor growth. Because of slower tumor growth, MH-85 tumor-bearing animals receiving injections of RG-13022 show less cachexia and hypercalcemia, eat more food, and are more active than untreated MH-85 tumor-bearing animals. As a result of suppression of tumor growth, RG-13022 prolongs the life span of MH-85 tumor-bearing animals. Administration of mAb108 i.p. (1 mg/mouse/day) at 1, 5, and 10 days after MH-85 inoculation of RG-13022 (400 μg/mouse/day) for 14 days profoundly inhibits MH-85 growth in nude mice.[1].
References

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